PKRA83 hydrochloride
PKRA83 (PKRA7) hydrochloride is a potent PK2 antagonist that competes for PK2 binding to its receptors, PKR1 and PKR2. PKRA83 hydrochloride potently inhibits PK2 receptors with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride exhibits anticancer, antiarthritis, and antiangiogenic activities.
For research use only. We do not sell to patients.
- Formula: C27H35Cl2FN2O4
- Molecular Weight:541.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 5.0 nM (PKR1) and 8.2 nM (PKR2)[1]
PKRA83 (1 µg/mL) hydrochloride effectively reduces PK2-induced microvascular endothelial cell branching in vitro[1].
PKRA83 (2 μM, 24 h) hydrochloride blocks the neuroprotective action of rPK2 in dopaminergic N27 cells (rPK2 protects N27 cell against MPP+-induced dopaminergic neuronal cell death)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PKRA83 (15 mg/kg; i.p, daily for 2 weeks) hydrochloride inhibits arthritis in mice with collagen-induced arthritis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model[1]
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Dosage:20 mg/kg
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Administration:i.p, daily
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Result:Decreased tumor growth rate and tumor weight.
Decreased relative blood vessel density and Increased areas of necrotic regions in tumors.
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Animal Model:Collagen-induced arthritis in mice[2]
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Dosage:15 mg/kg
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Administration:i.p, daily for 2 weeks
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Result:Showed less extensive inflammatory cell infiltration and synovial thickening in the joints (Histological evaluation).
Lowered IL-1β and 1 L-6 gene expression levels in the joints.
Chemical Information
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Molecular Weight 541.48
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Formula C27H35Cl2FN2O4
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SMILES
ClC1=C2C(OCCCO2)=CC(CN(CC(C)C)C([C@H]3CN(CC3)CC4=CC(OC)=C(C=C4)F)=O)=C1.Cl
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Synonyms
PKRA7 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Valerie F Curtis, et al. A PK2/Bv8/PROK2 antagonist suppresses tumorigenic processes by inhibiting angiogenesis in glioma and blocking myeloid cell infiltration in pancreatic cancer. PLoS One. 2013;8(1):e54916. [Content Brief]
[2]. Ito H, et al. Prokineticin 2 antagonist, PKRA7 suppresses arthritis in mice with collagen-induced arthritis. BMC Musculoskelet Disord. 2016 Sep 8;17(1):387. [Content Brief]
[3]. Gordon R, et al. Prokineticin-2 upregulation during neuronal injury mediates a compensatory protective response against dopaminergic neuronal degeneration. Nat Commun. 2016 Oct 5;7:12932. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PKRA83 hydrochloride Related Classifications
HY-147056B Related Classifications
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